Assay Detail
Binding
CHEMBL639639
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Inhibition of 1 nM [3H]- N6 -(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat fat cell membrane
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.21 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.22 |
| CHEMBL160369 | — | — | 1 | 8.89 |
| CHEMBL158507 | — | — | 1 | 8.23 |
| CHEMBL274855 | — | — | 1 | 7.44 |
| CHEMBL321505 | — | — | 1 | 7.39 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 6.46 |
| CHEMBL418333 | — | — | 1 | 6.37 |
| CHEMBL8488 | — | — | 1 | 5.82 |
| CHEMBL157655 | — | — | 1 | 5.80 |
| CHEMBL281811 | — | — | 1 | 5.70 |
| CHEMBL22042 | — | — | 1 | 5.38 |
| CHEMBL20483 | — | — | 1 | 5.31 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.06 |
| CHEMBL278332 | — | — | 1 | 4.92 |
| CHEMBL418375 | — | — | 1 | 4.83 |
| CHEMBL281633 | — | — | 1 | 4.48 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 4.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL160369 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL158507 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL274855 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL321505 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL418333 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL8488 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL157655 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL281811 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL22042 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL20483 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 8700.0 | nM | 5.06 |
| CHEMBL278332 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL418375 | — | Ki | = | 14900.0 | nM | 4.83 |
| CHEMBL281633 | — | Ki | = | 33000.0 | nM | 4.48 |
| CHEMBL113 | CAFFEINE | Ki | = | 59000.0 | nM | 4.23 |